Merck Sharp + Dohme Corp.

Merck + Co., Inc.

Other

Merck & Dohme Limited

Christopher Richard Moyes

Lihu Yang

Changyou Zhou

Michael Rowley

Alexander Pasternak

Gabor Butora

Gregori J Morriello

Stephen D Goble

Shankaran Kothandaraman

Richard Jiao

Sander G Mills

Timothy Harrison

Ian James Collins

Stephen Robert Fletcher

Alan John Nadin

Deodialsingh Guiadeen

Martin Richard Teall

Paul David Leeson

Timothy Jason Sparey

Cheng Tang

Leslie Joseph Street

Angus Murray MacLeod

Jose Luis Castro Pineiro

William Robert Carling

Richard Thomas Lewis

Andrew Pate Owens

Kevin William Moore

Graham A Showell

Gregory John Hollingworth

Alexander Richard Guiblin

Frank Burkamp

Peter Blurton

Edward Giles McIver

A Brian Jones

Lauren Rogers

Tracy Bayliss

The present invention is directed to compounds of the formula I: (wherein R, R, R, R, R, R, R, R, R, R, X, n and the dashed line are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptor CCR-2. The present invention is also directed to intermediates useful in the preparation of formula I compounds.

Tetrahydropyranyl cyclopentyl tetrahydropyridopyridine modulators of chemokine receptor activity

The present invention is directed to compounds of the formula I: Wherein R, R, R, R, R, R, R, R, R, X, n and the broken lines are as defined herein which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptor CCR-2.

Heterocyclic cyclopentyl tetrahydroisoquinoline and tetrahydropyridopyridine modulators of chemokine receptor activity

The present invention provides a compound of formula (I): wherein V represents NR, O, S, SO or S(O); W and X each independently represent CH or N; Y represents N, CH or C&#x2014;Ar, with the proviso that at least one, but no more than two, of W, X and Y are N; Z represents CH or C&#x2014;Ar, with the proviso that when Y is N or CH then Z is C&#x2014;Ar, and with the further proviso that when Y is C&#x2014;Arthen Z is CH; Arrepresents a fused 9 or 10 membered heterobicyclic ring system containing one, two, three or four heteroatoms selected from nitrogen, oxygen and sulfur, wherein at least one of the rings in said ring system is aromatic; Arrepresents an aromatic ring selected from phenyl, pyridyl, pyrimidinyl and pyridazinyl which is optionally fused and substituted; Rrepresents halogen, hydroxy, oxo, Calkyl, Calkenyl, Calkynyl, haloCalkyl, hydroxyCalkyl, Calkoxy, haloCalkoxy, hydroxyCalkoxy, Ccycloalkyl, Ccycloalkoxy, CcycloalkylCalkyl, cyano, nitro, SR, SOR, SOR, COR, NRCOR, CONRR, NRSOR, SONRR, &#x2014;(CH)carboxy, esterified &#x2014;(CH)carboxy or &#x2014;(CH)NRR; Rrepresents hydrogen, halogen, hydroxy, Calkyl, haloCalkyl, Ccycloalkyl, Calkoxy, haloCalkoxy, unsubstituted phenyl or phenyl substituted with one or two groups selected from halogen, Calkyl, haloCalkyl, Ccycloalkyl, Calkoxy or haloCalkoxy; Rand Rare each independently hydrogen, Calkyl, Calkenyl, Calkynyl, Ccycloalkyl or fluoroCalkyl; or Rand Rand the nitrogen atom to which they are attached together form a heteroaliphatic ring of 4 to 7 ring atoms, optionally substituted by one or two groups selected from hydroxy or Calkoxy, which ring may optionally contain as one of the said ring atoms an oxygen or a sulfur atom, S(O), S(O), or NR; Rrepresents hydrogen, Calkyl, hydroxyCalkyl or CalkoxyCalkyl; Rrepresents hydrogen, Calkyl, fluoroCalkyl, Ccycloalkyl, unsubstituted phenyl, or phenyl substituted with one or two groups selected from halogen, Calkyl, haloCalkyl, Ccycloalkyl, Calkoxy or haloCalkoxy; m is either zero or an integer from 1 to 4; n is either zero or an integer from 1 to 3; or a pharmaceutically acceptable salt, N-oxide or a prodrug thereof; a pharmaceutical composition comprising it; its use in methods of treatment; use of it for the manufacture of a medicament for treating VR-1 related conditions such as those in which pain and/or inflammation predominate; and methods of treatment using it. 

Amino-heterocycles as VR-1 antagonists for treating pain

The present invention is directed to methods for treating, preventing, ameliorating, controlling or reducing the risk of an inflammatory or immunoregulatory disorder or disease, which method comprises the administration to a patient of an effective amount of the compound of formula I: (wherein R, R, R, R, R, R, R, R, R, R, X, n and the dashed line are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptor CCR-2.

The present invention is directed to compounds of the formula I: I(wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, X, n and the dashed line are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptor CCR-2 

Tetrahydropyranyl cyclopentyl tetrahydroisoquinoline modulators of chemokine receptor activity

A class of substituted 1,2,4-triazolo&lsqb;4,3-&rsqb;pyridazine derivatives, possessing an optionally substituted cycloalkyl, phenyl or heteroaryl substituent at the 3-position, a substituted alkoxy moiety at the 6-position, and an optionally substituted bicycloalkyl ring system at the 7-position, are selective ligands for GABA receptors, in particular having high affinity for the &agr;2 and/or &agr;3 subunit thereof, and are accordingly of benefit in the treatment and/or prevention of disorders of the central nervous system, including anxiety and convulsions.

Imidazo-triazine derivatives as ligands for GABA receptors

Compounds according to Formula (I) or a salt thereof are selective antagonists of the human 5-HT2A receptor useful for treatment of adverse conditions of the central nervous system:

Phenylindole derivatives as 5-ht2a receptor ligands

Compounds according to Formula (I) or a salt thereof are selective ligands for GABA receptors useful for treatment of disorders of the central nervous system:

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Sawbridgeworth, United Kingdom

Christopher Richard Moyes